Rapid and efficient synthesis of 2-Amino-4H-benzothiazines

被引:50
作者
Hari, A [1 ]
Miller, BL [1 ]
机构
[1] Univ Rochester, Dept Chem, Rochester, NY 14627 USA
关键词
D O I
10.1021/ol006580m
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] The benzothiazine nucleus is a relatively unexplored class of compounds, from the standpoint of both synthetic chemistry and biological activity. We have developed a rapid, high yielding synthesis of benzothiazines in which a precursor aryl thiourea is prepared on solid phase, Addition of trifluoroacetic acid catalyzes a conjugate addition reaction to form the desired heterocycle and releases it from the resin.
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页码:3667 / 3670
页数:4
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